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Granular pharmaceutical compositions

a technology of pharmaceutical compositions and granules, applied in the field of granules, can solve the problems of difficult control, critical and difficult control, and continuous challenges of the process for the formulators

Inactive Publication Date: 2011-09-29
DR REDDYS LAB LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The granulated compositions exhibit improved blend homogeneity, consistent content uniformity, and controlled release profiles, enhancing the stability and efficacy of pharmaceutical formulations.

Problems solved by technology

But such processes pose continuous challenges to the formulators, as there can be a large difference in physical properties between the plurality of formulated particles and the excipients or granules used.
Size, shape and bulk density are a few physical properties that are critical and difficult to control.
These differences in physical properties may result in problems such as loss of blend homogeneity, poor compressibility and surface rupture of the formulated particles, leading to processing issues and differences in content uniformity, release profiles and stability of formulations.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0065]Tablet composition comprising metoprolol sustained release coated pellets co-granulated with Prosolv.

Grams / 1000IngredientTabletsDrug-SEAL-COATINGContainingDicalcium phosphate anhydrous (A-Tab) *33CoreEthyl cellulose 10 cPS4Acetyltributyl citrate1Isopropyl alcohol ‡481Methylene chloride ‡241DRUG-LOADINGMetoprolol succinate190Hydroxypropyl methylcellulose (HPMC)22Water ‡495Weight of drug-loaded pellet (mg)250SustainedEthyl cellulose120ReleaseHydroxypropylmethyl cellulose (HPMC)26CoatingAcetyltributyl citrate29Isopropyl alcohol ‡1050Methylene chloride ‡525Weight of SR coated pellet (A) (mg)425GranulationSilicified MCC (Prosolv HD 90) **416.27Hydroxypropyl cellulose (Klucel LF) ***40.53Water ‡400ExcipientHydroxypropyl cellulose (Klucel LF) ***30.00BlendCroscarmellose sodium23.5forSodium stearyl fumarate4.7TabletingFormulated tablet weight (B) (mg)940FilmHydroxypropyl methylcellulose (HPMC)16.56CoatingPolyethylene glycol 600024.82Talc2.06Titanium dioxide16.56Isopropyl alcohol ‡760M...

example 2

[0088]Evaluation of blends.

[0089]Tablet blends were evaluated for particle size distribution by sieve analysis. Loss on drying was determined at 105° C. Also the blends were analyzed for bulk density and metoprolol content.

[0090]To determine the content uniformity, a finished tablet was dispersed in water and pellets from the dispersion were separated by passing through a ASTM #40 mesh sieve. The pellets retained on the sieve were dried, and the weight of dried pellets from each tablet was recorded and expressed as % w / w as a measure of homogeneity of the blend. Ten tablets were tested for the content uniformity RSD calculation.

% w / wComparativeComparativeASTM MeshExample AExample BExampleTestingFractionBlendBlend1 BlendParticle SizeSR Coated Pellets#30 / #50909090DistributionProsolv or its#20 / #40050Granules (Neat#40 / #602352Prosolv for#60 / #80113011Example A and#80 / #100172017Example 1, andBelow701070granules of step 1#100in Example B)Lubricated Blend#30 / #50456575for Tableting#50 / #605141...

example 3

[0093]Comparative in vitro dissolution profiles (n=6) of metoprolol. succinate SR tablets from Comparative Examples A and B, and Example 1.

[0094]Procedure: Test 711 “Dissolution” in United States Pharmacopeia 29, United States Pharmacopeial Convention, Inc., Rockville, Md., 2005.

[0095]Medium: Phosphate buffer pH 6.8

[0096]Apparatus: USP Apparatus II (rotating paddle)

[0097]Volume: 500 ml

[0098]Rotation speed: 50 rpm

[0099]“Mean” values are cumulative percent of drug dissolved.

ComparativeComparativeTimeExample AExample BExample 1(hours)MeanRSD*MeanRSD*MeanRSD*000000013112.3188.5144.54478.5367.6333.88696.8564.6483.1201022.3982.1961.9*Relative standard deviation.

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PUM

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Abstract

Pharmaceutical compositions comprising a plurality of formulated particles containing at least one active ingredient and at least one pharmaceutically acceptable excipient, granulated with a granulating composition containing at least one pharmaceutical excipient.

Description

[0001]The present invention relates to granular compositions comprising a plurality of formulated particles, processes to prepare the compositions, and optionally converting such granular compositions into finished dosage forms.[0002]Various documents including U.S. Pat. Nos. 4,642,233, 5,643,602, 5,690,960, 5,753,265, 5,783,215, 5,910,319, and 6,136,344 disclose the preparation of pharmaceutical compositions such as tablets or capsules, comprising a plurality of formulated particles.[0003]Some pharmaceutical formulations contain a plurality of formulated particles comprising an active ingredient, or an active ingredient physically blended with inert ingredients, or an inert plurality of formulated particles, filled into capsules, or the plurality of formulated particles are physically blended with pharmaceutically acceptable excipients or inert granules and such blends are compressed into tablets, as is known in processes for preparing formulations using a plurality of formulated p...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/48A61K9/50A61K31/445A61K9/20A61P37/08B05D5/00B05D7/00
CPCA61K9/2077A61K9/5078A61K9/2866A61K9/284
Inventor PASHA, MOHAMMAD BALAKANDARAPU, RAGHUPATHISHETTY, VASANTH KUMARBHUSHAN, INDUMOHAN, MAILATUR SIVARAMAN
Owner DR REDDYS LAB LTD
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